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  • Title: Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
    Author: Zhang JQ, Luo YJ, Xiong YS, Yu Y, Tu ZC, Long ZJ, Lai XJ, Chen HX, Luo Y, Weng J, Lu G.
    Journal: J Med Chem; 2016 Aug 11; 59(15):7268-74. PubMed ID: 27427973.
    Abstract:
    Three series of substituted pyrimidines were designed and synthesized. All target compounds were screened for kinase inhibitory activities against PI3Kα, and most IC50 values were found within the nanomolar range. Compounds 5d and 5p displayed comparable activities relative to the positive control 5a. 5p also showed a significant isozyme selectivity (PI3Kβ/α). Furthermore, the cytotoxicities of these pyrimidines against human cancer cell lines were evaluated and the in vivo anticancer effect of 5d was also tested.
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